Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027960 (mole)
 21,279 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A novel purine, (N6-2-(4-chlorophenyl)-bicyclo 2.2.2.-octyl-(3)-adenosine) EMD 28422 increases the binding of (3H) diazepam to benzodiazepine receptors in vivo within 10 min after intraperitoneal administration. This increase in (3H) diazepam binding is due to an increase in the number of benzodiazepine receptors (Bmax) rather than an altered affinity of the radioligand for receptor (Kd), EMD 28422 protects mice against pentylenetetrazole and caffeine-induced seizures and potentiates the anticonvulsant action of subeffective doses of diazepam in a dose-dependent fashion. Furthermore, EMD 28422 also produces a significant increase in punished responding in a conflict situation (rats), and a long-lasting, dose-dependent decrease in spontaneous motor activity (mice). In contrast, neither EMD 39011 nor adenosine (the two component molecules of EMD 28422) possess anticonvulsant properties at doses up to five mole-equivalents of EMD 28422. These data indicate that the purine EMD 28422 produces a spectrum of pharmacologic effects similar to the benzodiazepines, yet in contrast to the benzodiazepines (and other purines), increases benzodiazepine receptor number. Thus, EMD 28422 may represent the prototype of a class of synthetic purines exerting a unique neurochemical effect on benzodiazepine receptors and possessing several therapeutic actions of the benzodiazepines.
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PMID:Pharmacologic and behavioral effects of EMD 28422: a novel purine which enhances (3H) diazepam binding to brain benzodiazepine receptors. 739 62

Electronic absorption and emission spectra of 10-bis(phenylethynyl)anthracene (PEA) and coumarin 153 (C153) are measured as functions of composition along the bubble-point curve at 25 degrees C in CO2-expanded cyclohexane (c-C6H12), acetonitrile (CH3CN), and methanol (CH3OH). The nonlinear dependence of the spectral frequencies on composition suggests substantial preferential solvation of both solutes by the liquid components of these mixtures. Estimates of enrichment factors (local mole fraction of a component divided by its bulk value) based on the assumption that spectral shifts are linearly related to local composition are quite large (approximately 10) in the cases of the C153/CH3CN + CO2 and C153/CH3OH + CO2 systems at high xCO2. Computer simulations of anthracene, the chromophore of PEA, and C153 in these three CO2-expanded liquids are used to clarify the relationship between local composition and spectral shift. A semiempirical model consisting of additive electrostatic and dispersive interactions is able to capture the main features observed experimentally in all six solute/solvent combinations. The simulations show that the commonly used assumption of a linear relation between spectral shifts and local compositions grossly exaggerates the extent of preferential solvation in these mixtures. The collective nature of electrostatic solvation and the composition dependence of the solute's coordination number are shown to be responsible for the breakdown of this assumption.
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PMID:Solvation and solvatochromism in CO2-expanded liquids. 2. Experiment-simulation comparisons of preferential solvation in three prototypical mixtures. 1738 63